公开(公告)号：US06235789B1

公开(公告)日：2001-05-22

申请号：US08530148

申请日：1997-05-28

申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Masaomi Miyamoto

IPC分类号： A61K3116

CPC分类号： C07C271/16 ,  C07C233/18 ,  C07C233/20 ,  C07C233/36 ,  C07C233/60 ,  C07C233/73 ,  C07C235/08 ,  C07C235/48 ,  C07C275/24 ,  C07C275/34 ,  C07C2601/02 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07C2603/94 ,  C07D211/62

摘要： A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.

摘要翻译： 式R 1和R 2的化合物是H，烃基或杂环基，或R 1和R 2组合​​成螺环; R3是烃基，取代氨基，取代羟基或杂环基; R4是H或烷基; 环A是取代的苯环; m和n表示1至4; {overscore（.........）}是指单键或双键或其盐，其制备方法和具有对褪黑激素受体的结合亲和力的组合物。

公开(公告)号：US5922771A

公开(公告)日：1999-07-13

申请号：US693058

申请日：1996-08-19

申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

IPC分类号： C07C233/18 ,  C07C271/06 ,  C07D317/70 ,  A61K31/16 ,  A61K31/165 ,  A61K31/27 ,  A61K31/335 ,  C07C233/64 ,  C07C235/00 ,  C07C237/00

CPC分类号： C07C233/18 ,  C07C271/06 ,  C07C2102/08

摘要： A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

摘要翻译： PCT No.PCT / JP96 / 02091 Sec。 371日期：1996年8月19日 102（e）日期1996年8月19日PCT提交1996年7月25日PCT公布。 公开号WO97 / 05098 日期：1997年2月13日下式化合物其中R 1和R 2独立地表示H或任选取代的烃基; R3表示任选取代的烃基; R4表示H或烃基; 环A表示取代的苯环; X表示C2-4亚烷基等; Y表示键或低级亚烷基，或其盐可用作与褪黑激素相关的疾病的预防或治疗剂。

公开(公告)号：US07208495B2

公开(公告)日：2007-04-24

申请号：US10481367

申请日：2002-07-04

申请人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

发明人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

IPC分类号： A61K31/497 ,  A61K31/445 ,  C07D405/00 ,  C07D401/00

CPC分类号： A61K31/4525 ,  A61K31/496 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D307/82 ,  C07D307/83 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/14

摘要： A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3–8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5–8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and— represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.

摘要翻译： 由下式表示的化合物（其中，R 1和R 2相同或不同，各自表示氢原子，烃基或杂环基， 可以与相邻的碳原子一起形成3-8元的异或杂环基，R 3表示环状 基团，羟基，可具有氧代基的巯基或氨基，R 4表示氢原子，烃基，羟基，可具有氧代基的巯基，或 氨基或R 2和R 4可以连接在一起形成双键，X表示键或直链烃基，W表示氧原子或 硫原子，环B表示5-8元含氮杂环基，环C表示苯环，代表单键或双键）或其盐或前药具有优异的神经变性抑制活性， 脑穿透性 并且可用作预防/治疗神经变性疾病的药剂。

公开(公告)号：US06218429B1

公开(公告)日：2001-04-17

申请号：US09309519

申请日：1999-05-10

申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

IPC分类号： A01N34308

CPC分类号： C07D263/52 ,  C07D265/34 ,  C07D307/93 ,  C07D311/94 ,  C07D317/70 ,  C07D319/14 ,  C07D491/04 ,  Y10S514/923

摘要： A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

摘要翻译： 下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

公开(公告)号：US6034239A

公开(公告)日：2000-03-07

申请号：US812168

申请日：1997-03-06

申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

IPC分类号： C07C233/00 ,  C07D307/92 ,  C07D413/00 ,  C07D493/00

CPC分类号： C07D307/77 ,  C07D263/62 ,  C07D311/94 ,  C07D317/70 ,  C07D319/14 ,  C07D491/04

摘要： A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

摘要翻译： 下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

公开(公告)号：US20070149558A1

公开(公告)日：2007-06-28

申请号：US11679257

申请日：2007-02-27

申请人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

发明人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

IPC分类号： A61K31/4747 ,  A61K31/407

CPC分类号： A61K31/4525 ,  A61K31/496 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D307/82 ,  C07D307/83 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/14

摘要： A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3-8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5-8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.

摘要翻译： 由下式表示的化合物（其中，R 1和R 2相同或不同，各自表示氢原子，烃基或杂环基， 可以与相邻的碳原子一起形成3-8元的异或杂环基，R 3表示环状 基团，羟基，可具有氧代基的巯基或氨基，R 4表示氢原子，烃基，羟基，可具有氧代基的巯基，或 氨基或R 2和R 4可以连接在一起形成双键，X表示键或直链烃基，W表示氧原子或 硫原子，环B表示5-8元含氮杂环基，环C表示苯环，并且表示单键或双键）或其具有优异的神经变性抑制活性和脑渗透性的盐或其前药，并且可用作预防/治疗神经变性疾病的药剂。

公开(公告)号：US20060241168A1

公开(公告)日：2006-10-26

申请号：US11475539

申请日：2006-06-27

申请人： Shigenori Ohkawa ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Masaomi Miyamoto

IPC分类号： A61K31/4035 ,  C07D405/02

CPC分类号： C07D405/04 ,  C07D307/79 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D491/10

摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.

摘要翻译： 一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R 1和R 2：H，烃基或杂环基或R 与相邻的碳原子一起形成环;和<！ - SIPO

公开(公告)号：US06348485B1

公开(公告)日：2002-02-19

申请号：US09700405

申请日：2000-11-14

申请人： Shigenori Ohkawa ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Masaomi Miyamoto

IPC分类号： A61K31415

CPC分类号： A61K31/435 ,  A61K31/495 ,  A61K31/55 ,  A61K2300/00

摘要： The present invention provides a pharmaceutical composition for treating or preventing sleep disorders which comprises (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide in combination with at least one active component selected from zolpidem, zopiclone, triazolam and brotizolam.

摘要翻译： 本发明提供了用于治疗或预防睡眠障碍的药物组合物，其包含（S）-N- [2-（1,6,7,8-四氢-2H-茚并[5,4-b]呋喃-8-基 ）乙基]丙酰胺与至少一种选自唑吡旦，佐匹克隆，三唑仑和brotizolam的活性成分组合。

公开(公告)号：US07750037B2

公开(公告)日：2010-07-06

申请号：US11475539

申请日：2006-06-27

申请人： Shigenori Ohkawa ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Masaomi Miyamoto

IPC分类号： A61K31/4035 ,  C07D405/02

CPC分类号： C07D405/04 ,  C07D307/79 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D491/10

摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.

摘要翻译： 一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R1和R2：H，烃基或杂环基或R1和R2与相邻碳原子一起形成环; R3：H，烃基或杂环基; W：表示由下式表示的基团：其中环A：任选取代的苯环; 环B：任选取代的5-至7-元含氮杂环; R4：被芳基取代并进一步任选取代的脂族烃基或含芳基的酰基; R5：H，C1-6烷基或酰基; R4c：芳基，脂族烃基或酰基; 和X：O或S; Y：O，S或NH; 和环C：任选取代的苯环，或其盐或前药，并且提供了用于预防或治疗抑郁，焦虑，躁狂抑郁性精神病或PTSD的活化剂。

公开(公告)号：US20050148650A1

公开(公告)日：2005-07-07

申请号：US10506269

申请日：2003-02-28

申请人： Shigenori Ohkawa ,  Masaomi Miyamoto

发明人： Shigenori Ohkawa ,  Masaomi Miyamoto

IPC分类号： A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D307/79 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D491/056 ,  C07D491/10 ,  C07D491/107 ,  A61K31/4035 ,  A61K31/407

CPC分类号： C07D405/04 ,  C07D307/79 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D491/10

摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X:O or S; Y:O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.

摘要翻译： 一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R 1和R 2：H，烃基或杂环基或R 与相邻的碳原子一起形成环;和<！ - SIPO